Art. -Nr.: HY-B1392

Esmolol hydrochloride

3 Cited Publications

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Esmolol hydrochloride is an ultra-short-acting cardioselective β1-adrenergic blocker. Esmolol hydrochloride exerts its antiarrhythmic effect by activating Neurokinin 1 Receptor. Esmolol hydrochloride attenuates post resuscitation myocardial dysfunction. Esmolol hydrochloride improves diabetic wound healing by inhibiting aldose reductase and the production of advanced glycation end products and promoting fibroblast migration. Esmolol hydrochloride can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers.

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Reinheit: 99.69%
CAS. Nr.: 81161-17-3
Formel: C₁₆H₂₆ClNO₄
Molecular Weight:331.83

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Esmolol hydrochloride Chemical Structure

CAS. Nr.: 81161-17-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1][2][3]

β-adrenoceptor

Caspase 3

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Alle Neurokinin Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Esmolol hydrochloride (0-1 mM) inhibits aldose reductase activity with an estimated IC₅₀ of 150 µM, and inhibits sorbitol formation in red blood cells by 59%^[1].
Esmolol hydrochloride (0.5-1 mM, 10 min) inhibits the formation of advanced glycation end products (AGEs)^[1].
Esmolol hydrochloride (0.01- 1000 μM, 8-48 h) can promote the ability to migrate and has non-cytotoxic in HFF-1, Ea.hy926 and HaCaT cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Migration Assay ^[1]

Cell Line:

HFF-1, Ea.hy926, HaCaT cells
Concentration:

0.01 μM, 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM, 500 μM, 100 μM
Incubation Time:

8 h, 14 h, 16 h, 22 h, 24 h, 42 h, 48 h
Result:

Promoted the ability to migrate, with low migration at 100 and 500 µM.

In Vivo

Esmolol hydrochloride (7%-20%, topical applied, twice daily) improves NO induction, collagen turnover, and hydroxyproline levels, remodeling and wound healing in Streptozotocin (HY-13753)-induced diabetic hairless rats^[1].
Esmolol (10 mg/kg, in 0.3 mL, i.v., once) hydrochloride shows anti-arrhythmic effect via up-egulation of NK1 receptor in permanent coronary artery occlusion (CAO) rat model^[2].
Esmolol (300 μg/kg with Epinephrine 20 μg/kg, i.v., once) hydrochloride protects myocardial tissue and improves post-resuscitation myocardial dysfunction by reducing apoptosis in inbred wuzhishan miniature pigs^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Streptozotocin-induced (35 mg/kg/day for 5 consecutive days) diabetic hairless rats model^[1]
Dosage:

7, 14, and 20%
Administration:

topical applied, twice daily
Result:

Increased the total nitrite content and NO level in wound tissue by 44% and 112% in the G14 group compared with the diabetic control group and the vehicle control group, and by 8% and 59% in the G20 group compared with the diabetic control group and the vehicle control group.
Improved collagen content, hydroxyproline levels, increased hydroxyproline levels by 22% and 44% in the G14 group, and 21% and 43% in the G20 on day 7; increased hydroxyproline levels by 6% and 13% in the G14 group, increased hydroxyproline levels by 41% and 49% in the G20 group on day 14, compared with the diabetic control and vehicle control groups.
Improved healing in G20 group and closer to normal intact diabetic skin (wounds were not completely closed on day 19) .

Animal Model:

CAO male SD rats (weighing 260-280 g) model^[2]
Dosage:

10 mg/kg, in 0.3 mL
Administration:

i.v., once
Result:

Reduced ventricular ectopic beat (VEB) by 66%, and reduced the incidence, number, and duration of VT and VF by 66%, 92%, and 95%, respectively .
Attenuated the arrhythmogenic effects of D-SP, reducing the VEB by 45%, the morbidity rate, the episodes and the durations of VT & VF by 86%, 62% and 50% respectively, in 9-23 min following the coronary artery occlusion (CAO) (14 min-28 min after the injection of esmolol).
Increased NK1-R mRNA and protein, by 72% and 19% respectively, at 15 min after the CAO.

Animal Model:

Inbred wuzhishan miniature pigs (12-14 months of age, 30 kg) model^[3]
Dosage:

300 μg/kg with Epinephrine (HY-B0447B) 20 μg/kg
Administration:

i.v., once
Result:

Reduced the number of shocks, defibrillation energy, return of spontaneous circulation (ROSC) time and 4 h heart rate (HR), and increased the 24 h survival rate, 4-6 h CO values, 4 h mean aortic pressure (MAP) value, and 4 h left ventricular dp/dtmax.
Reduced serum cTnI, lactate concentrations and , myocardial malondialdehyde (MDA) content, increased ATPase and SOD levels.
Reduced caspase-3 proteolytic activation, mRNA levels, and TUNEL-positive cells, and attenuated apoptotic effects by upregulating Bcl-2/Bax protein levels.

Chemical Information

CAS. Nr. 81161-17-3
Appearance Solid
Molecular Weight 331.83
Formel C₁₆H₂₆ClNO₄
Color White to off-white
SMILES

O=C(OC)CCC1=CC=C(OCC(O)CNC(C)C)C=C1.[H]Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (3)

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2019 Dec;65(12):1522-1531. PMID: 31578215
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2022 Jun 7;23(6):e53932. PMID: 35403787
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Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]

2021 Feb 20:195:113870. PMID: 33453569

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (301.36 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 50 mg/mL (150.68 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0136 mL

15.0680 mL

30.1359 mL

5 mM

0.6027 mL

3.0136 mL

6.0272 mL

10 mM

0.3014 mL

1.5068 mL

3.0136 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.75 mg/mL (8.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.75 mg/mL (8.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.75 mg/mL (8.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 100 mg/mL (301.36 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
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- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kulkarni SA, et al. Novel topical esmolol hydrochloride improves wound healing in diabetes by inhibiting aldose reductase, generation of advanced glycation end products, and facilitating the migration of fibroblasts. Front Endocrinol (Lausanne). 2022 Aug 23;13:926129. [Content Brief]

[2]. Wang LL, et al. Esmolol activates endogenous neurokinin activity inhibiting infarction-induced arrhythmias in rats: novel mechanisms of anti-arrhythmia. Regul Pept. 2013 Sep 10;186:116-22. [Content Brief]

[3]. Zhang Q, et al. Combination of epinephrine with esmolol attenuates post-resuscitation myocardial dysfunction in a porcine model of cardiac arrest. PLoS One. 2013 Dec 18;8(12):e82677. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	3.0136 mL	15.0680 mL	30.1359 mL	75.3398 mL
	5 mM	0.6027 mL	3.0136 mL	6.0272 mL	15.0680 mL
	10 mM	0.3014 mL	1.5068 mL	3.0136 mL	7.5340 mL
	15 mM	0.2009 mL	1.0045 mL	2.0091 mL	5.0227 mL
	20 mM	0.1507 mL	0.7534 mL	1.5068 mL	3.7670 mL
	25 mM	0.1205 mL	0.6027 mL	1.2054 mL	3.0136 mL
	30 mM	0.1005 mL	0.5023 mL	1.0045 mL	2.5113 mL
	40 mM	0.0753 mL	0.3767 mL	0.7534 mL	1.8835 mL
	50 mM	0.0603 mL	0.3014 mL	0.6027 mL	1.5068 mL
	60 mM	0.0502 mL	0.2511 mL	0.5023 mL	1.2557 mL
	80 mM	0.0377 mL	0.1883 mL	0.3767 mL	0.9417 mL
	100 mM	0.0301 mL	0.1507 mL	0.3014 mL	0.7534 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Esmolol hydrochloride

3 Cited Publications

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Esmolol hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Esmolol hydrochloride

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Alle Neurokinin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Esmolol hydrochloride Related Classifications

HY-B1392 Related Classifications